Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery

Inhibitors targeting the general RNA polymerase II (RNAPII) transcription machinery are candidate therapeutics in cancer and other complex diseases. Here, we review the molecular targets and mechanisms of action of these compounds, framing them within the steps of RNAPII transcription. We discuss th...

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Main Authors:	Ryan D. Martin, Terence E. Hébert, Jason C. Tanny
Format:	Article
Language:	English
Published:	MDPI AG 2020-05-01
Series:	International Journal of Molecular Sciences
Subjects:	RNA polymerase II transcription CDK inhibitor CDK7 CDK9 CDK12
Online Access:	https://www.mdpi.com/1422-0067/21/9/3354

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spelling	doaj-d730a48df81d47309df49b9a5340fa6e2020-11-25T03:51:41ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672020-05-01213354335410.3390/ijms21093354Therapeutic Targeting of the General RNA Polymerase II Transcription MachineryRyan D. Martin0Terence E. Hébert1Jason C. Tanny2Department of Pharmacology and Therapeutics, McGill University, Montreal, QC H3G 1Y6, CanadaDepartment of Pharmacology and Therapeutics, McGill University, Montreal, QC H3G 1Y6, CanadaDepartment of Pharmacology and Therapeutics, McGill University, Montreal, QC H3G 1Y6, CanadaInhibitors targeting the general RNA polymerase II (RNAPII) transcription machinery are candidate therapeutics in cancer and other complex diseases. Here, we review the molecular targets and mechanisms of action of these compounds, framing them within the steps of RNAPII transcription. We discuss the effects of transcription inhibitors in vitro and in cellular models (with an emphasis on cancer), as well as their efficacy in preclinical and clinical studies. We also discuss the rationale for inhibiting broadly acting transcriptional regulators or RNAPII itself in complex diseases.https://www.mdpi.com/1422-0067/21/9/3354RNA polymerase IItranscriptionCDK inhibitorCDK7CDK9CDK12
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Ryan D. Martin Terence E. Hébert Jason C. Tanny
spellingShingle	Ryan D. Martin Terence E. Hébert Jason C. Tanny Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery International Journal of Molecular Sciences RNA polymerase II transcription CDK inhibitor CDK7 CDK9 CDK12
author_facet	Ryan D. Martin Terence E. Hébert Jason C. Tanny
author_sort	Ryan D. Martin
title	Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery
title_short	Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery
title_full	Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery
title_fullStr	Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery
title_full_unstemmed	Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery
title_sort	therapeutic targeting of the general rna polymerase ii transcription machinery
publisher	MDPI AG
series	International Journal of Molecular Sciences
issn	1661-6596 1422-0067
publishDate	2020-05-01
description	Inhibitors targeting the general RNA polymerase II (RNAPII) transcription machinery are candidate therapeutics in cancer and other complex diseases. Here, we review the molecular targets and mechanisms of action of these compounds, framing them within the steps of RNAPII transcription. We discuss the effects of transcription inhibitors in vitro and in cellular models (with an emphasis on cancer), as well as their efficacy in preclinical and clinical studies. We also discuss the rationale for inhibiting broadly acting transcriptional regulators or RNAPII itself in complex diseases.
topic	RNA polymerase II transcription CDK inhibitor CDK7 CDK9 CDK12
url	https://www.mdpi.com/1422-0067/21/9/3354
work_keys_str_mv	AT ryandmartin therapeutictargetingofthegeneralrnapolymeraseiitranscriptionmachinery AT terenceehebert therapeutictargetingofthegeneralrnapolymeraseiitranscriptionmachinery AT jasonctanny therapeutictargetingofthegeneralrnapolymeraseiitranscriptionmachinery
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Therapeutic Targeting of the General RNA Polymerase II Transcription Machinery

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